Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives.
The synthesis and biological evaluation of a series of diphenyl ether derivatives were described. The compounds can either activate or inhibit the aminopeptidase activity of leukotriene A(4) hydrolase, while at the same time do not influence the hydrolase activity. Further enzyme kinetics and molecular modeling investigation on these novel chemical activators revealed their possible activation mechanism. These compounds can be used as probes to regulate the aminopeptidase activity of leukotriene A(4) hydrolase.
Jiang
Xiaolu
X
Beijing National Laboratory for Molecular Sciences, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
Zhou
Lu
L
Wei
Dengguo
D
Meng
Hu
H
Liu
Ying
Y
Lai
Luhua
L
D002626:Chemistry, Pharmaceutical; D015195:Drug Design; D004789:Enzyme Activation; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D006801:Humans; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D010647:Phenyl Ethers / Q000737:chemistry*; D011485:Protein Binding; D013379:Substrate Specificity
D010647:Phenyl Ethers; C031538:phenyl ether; D004851:Epoxide Hydrolases; C043134:leukotriene A4 hydrolase